专利号:US-8735586-B2 优先权日:2007-06-26 标 题 :Regioselective copper catalyzed synthesis of benzimidazoles and azabenzimidazoles 发明人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARÉ MARC; URMANN MATTHIAS; HALLAND NIS; RKYEK OMAR 权利人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARÉ MARC; URMANN MATTHIAS; HALLAND NIS; RKYEK OMAR; SANOFI SA 摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula I, n nwherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4, Q and J have the meanings indicated in the claims. The present invention provides a direct copper catalyzed regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides.
专利号:US-8188282-B2 优先权日:2006-07-15 标 题:Regioselective palladium catalyzed synthesis of benzimidazoles and azabenzimidazoles 发明人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARE MARC; HALLAND NIS; RKYEK OMAR; URMANN MATTHIAS 权利人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARE MARC; HALLAND NIS; RKYEK OMAR; URMANN MATTHIAS; SANOFI AVENTIS 摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula I, n nwherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4, Q and J have the meanings indicated in the claims. The present invention provides a direct palladium catalyzed, regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides useful for the production of pharmaceuticals, diagnostic agents, liquid crystals, polymers, herbicides, fungicidals, nematicidals, parasiticides, insecticides, acaricides and arthropodicides.
专利号:US-7151112-B1 优先权日:2001-09-04 标题:Pharmaceutical uses and synthesis of nicotinamides 发明人:CUTSHALL NEIL S; JEFFREY SCOTT C 权利人:UCB SA 摘要:This invention is directed to methods of using a compound of the formula n nand pharmaceutically acceptable salts thereof, wherein n, X, R 1 and R 2 are disclosed herein, for treating inflammatory events in an animal subject.
专利号:US-2010261909-A1 优先权日:2007-06-26 标题 :Regioselective copper catalyzed synthesis of benzimidazoles and azabenzimidazoles
专利号:WO-02053544-A1 优先权日:2000-12-29 标题 :Pharmaceutical uses and synthesis of nicotinanilide-n-oxides
专利号:WO-2009000413-A1 优先权日:2007-06-26 标题:A regioselective copper catalyzed synthesis of benzimidazoles and azabenzimidazoles
参考标题:Copper-Catalyzed Regioselective Synthesis OfN-Aryl Amides From Aldoximes And Aryl Halides 作者:Niranjan Panda,Raghavender Mothkuri,Dinesh Kumar Nayak |发布日期:2014.3 摘要:Ligand-Assisted Copper-Catalyzed Reaction Of Aldoximes With Aryl Halides Is Described For The Regioselective Synthesis Of N-Aryl Amides. This Protocol Is Simple And Compatible With A Wide Range Of Functional Groups Attached To The Aryl Ring Of The Halides As Well As Aldoximes.
合成参考文献
摘要:Neumann, H.; Schranck, J., Science of Synthesis: C-1 Building Blocks in Organic Synthesis, (2013) 2, 74. 摘要:Nakao, Y., Science of Synthesis: Catalytic Transformations via CH Activation, (2015) 1, 367. 摘要:Li, H.; Wang, Y.; Liu, Q., Science of Synthesis: Base-Metal Catalysis, (2023) 2, 551. 参考文献:10.1038/nchem.1506 摘要:Over B, Wetzel S, Grütter C, Nakai Y, Renner S, Rauh D, Waldmann H. Natural-product-derived fragments for fragment-based ligand discovery. Nat Chem. 2013 Jan;5(1):21–8. doi: 10.1038/nchem.1506.